Detailed description page of THPdb

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1609 details

Primary information
ThPP ID	Th1132
Therapeutic Peptide/Protein Name	Belimumab
Sequence	N.A. view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	147000
Chemical Formula	C 6358 H 9904 N 1728 O 2010 S 44
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	Elimination half life- 19.4 days, Distribution half life- 1.75 days
Description	RAV12 is a monoclonal antibody that is being studied in the treatment of certain cancers.It binds to a carbohydrate molecule found on gastric, colon, pancreatic, prostate, ovarian, breast, and kidney cancer cells. Administering RAV12 along with gemcitabine may kill more tumor cells than either one alone.
Indication/Disease	Adjunct treatment for auto-antibody-positive active systemic lupus erythematosus.
Pharmacodynamics	By the 52nd week of treatment with belimumab, a reduction in CD19+, CD20+, naive and activated B cells, plasma cells, plasmacytoid cells, and SLE B-cell subset can be observed. Reductions in plasma cells and SLE B-cell subset can be seen by the eighth week and these levels were maintained to week 52. Belimumab also reduced levels of IgG and anti-dsDNA.
Mechanism of Action	Belimumab selectively binds to soluble human B lymphocyte stimulator protein (BLyS) so that BLyS is unable to bind to receptors on B lymphocytes. The binding of BLyS to its receptor is essential for the survival of B lymphocytes. Consequently, belimumab reduces B-cell mediated immunity and the autoimmune response.
Toxicity	The most commonly-reported adverse reactions, occurring in â‰¥ 5% of patients in clinical trials were nausea, diarrhea, pyrexia, nasopharyngitis, bronchitis, insomnia, pain in extremity, depression, migraine, and pharyngitis. The most common serious adverse reactions were serious infections.
Metabolism	Because belimumab is a protein, it is expected that it is degraded into peptides and amino acids by proteolytic enzymes.
Absorption	Cmax, 10 mg/kg, SLE patients = 313 Âµg/mL; AUC (0 - âˆž), 10 mg/kg, SLE patients = 3083.
Volume of Distribution	Vdss, 10 mg/kg, SLE patients = 5.29 L.
Clearance	Systemic clearance, 10 mg/kg, SLE patients = 215 mL/day.
Categories	Monoclonal antibodies
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	Tumor necrosis factor ligand superfamily member 13B
Information of corresponding available drug in the market
Brand Name	Benlysta
Company	GlaxoSmithKline
Brand Discription	BENLYSTA (belimumab) is a human IgG1Î» monoclonal antibody specific for soluble human B lymphocyte stimulator protein (BLyS, also referred to as BAFF and TNFSF13B). Belimumab has a molecular weight of approximately 147 kDa. Belimumab is produced by recombinant DNA technology in a mammalian cell expression system.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	Upon reconstitution with Sterile Water for Injection, USP, each single-use vial delivers 80 mg/mL belimumab in 0.16 mg/mL citric acid, 0.4 mg/mL polysorbate 80, 2.7 mg/mL sodium citrate, and 80 mg/mL sucrose, with a pH of 6.5.
Physcial Appearnce	BENLYSTA is supplied as a sterile, white to off-white, preservative-free, lyophilized powder for Intravenous infusion
Route of Administration	Intravenous infusion
Recommended Dosage	10 mg/kg at 2-week intervals for the first 3 doses and at 4-week intervals thereafter. Reconstitute, dilute, and administer as an Intravenous infusion only, over a period of 1 hour.
Contraindication	anaphylaxis with belimumab
Side Effects	Mortality, Serious Infections, Malignancy, Hypersensitivity Reactions, Including Anaphylaxis, Infusion Reactions, Depression
Useful Link	http://www.rxlist.com/benlysta-drug.htm http://www.benlysta.com/ http://en.wikipedia.org/wiki/Belimumab
PubMed ID	25652332, 25609919, 25543845, 22428610
3-D Structure	N.A.